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Epigenetic Reader Domain
Catalog No. | Inhibitor Name | Epigenetic Reader Domain |
---|---|---|
A12729 | (*)-JQ1 | *** |
A11783 | I-BET151 | * |
A12545 | PFI-1 | ** |
A11440 | I-BET-762 | *** |
A13956 | RVX-208 | * |
A13227 | SGC-CBP30 | **** |
A13163 | Bromosporine | **** |
A13890 | OTX015 | **** |
A12948 | UNC1215 | ** |
A13717 | UNC669 | * |
A14133 | GSK1324726A | *** |
A13749 | MS436 | ** |
A13068 | CPI-203 | *** |
A13957 | PFI-3 |
Notes:
1.Hover mouse over " " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
Catalog No. | Product Name | Application | Product Information |
---|---|---|---|
A11783 SALE |
GSK 1210151A (I-BET151) |
BET Bromodomain 抑制剂 |
GSK1210151A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4.
|
A16196 SALE |
BI-9564 |
BRD7/9 抑制剂 |
BI-9564 is a potent and selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 uM, respectively).
|
A16068 |
BI-7273 |
BRD9 BD 抑制剂 |
BI-7273 is a selective, and cell-permeable BRD9 BD inhibitor.
|
A15872 |
I-BRD9 |
Selective BRD9 抑制剂 |
I-BRD9 is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4.
|
A13749 |
MS436 |
BRD4 抑制剂 |
MS436 is a diazobenzene-based small-molecule inhibitor for the BRD4 bromodomains with a Ki value of 30-50 nM.
|
A13165 SALE |
I-CBP112 |
CBP/p300 bromodomain 抑制剂 |
I-CBP112 is a highly potent and selective p300/CBP bromodomain inhibitor (IC50 ~0.14-0.17 uM for CBP and ~0.625 uM for p300).
|
A12948 SALE |
UNC1215 |
L3MBTL3 抑制剂 |
UNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity.
|
A13890 SALE |
OTX015 |
BET 抑制剂 |
OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).
|
A13227 |
SGC-CBP30 |
CBP/p300 bromodomain 抑制剂 |
SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators.
|
A12545 SALE |
PFI-1 |
BET 抑制剂 |
PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4.
|
A11440 SALE |
GSK 525762A (I-BET-762) |
BET 抑制剂 |
GSK-525762A is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family
|
A13068 |
CPI-203 |
BET bromodomain 抑制剂 |
CPI203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay).
|
A13163 SALE |
Bromosporine |
bromodomain 抑制剂 |
Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.
|
A13717 |
UNC 669 |
L3MBTL 抑制剂 |
UNC669 is a small-molecule antagonist of methyl-lysine (KMe) reader protein with selectivity for L3MBTL1 and L3MBTL3 (IC50 of 4.2μM and 3.1μM respectively)
|
A12729 SALE |
(+)-JQ1 |
BET 抑制剂 |
(+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor.
|
A15947 |
BAZ2-ICR |
BAZ2 bromodomain 抑制剂 |
BAZ2-ICR is an excellent chemical probe for functional studies of the BAZ2 bromodomains in vitro and in vivo.
|
A16000 |
OF-1 |
BRPF1B/BRPF2 bromodomain 抑制剂 |
OF-1 is a chemical probe for BRPF bromodomains. OF-1 has been shown to bind to BRPF1B with a KD of 100 nM (ITC), to BRPF2 with a KD of 500 nM (ITC) and to BRPF3 with a KD of 2.4 uM (ITC).
|
A16076 |
CPI 0610 |
BET bromodomain 抑制剂 |
CPI 0610 is a small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity.
|
A16092 |
GSK 5959 |
BRPF1 bromodomain 抑制剂 |
GSK 5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM. Exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.
|
A16180 |
EML 425 |
CBP/p300 抑制剂 |
EML 425 is a reversible and non-competitive CBP/p300 inhibitor that is cell permeable (IC50 values are 1.1 and 2.9 uM, respectively).
|
A16330 |
GSK6853 |
BRPF1 bromodomain 抑制剂 |
GSK6853 is a potent and selective inhibitor of the BRPF1 bromodomain. shows excellent BRPF1 potency (pKd 9.5) and greater than 1600-fold selectivity over all other bromodomains tested.
|
A16355 |
CeMMEC13 |
TAF1 抑制剂 |
CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 μM).
|
A16366 |
OXF BD 02 |
BRD4 抑制剂 |
OXF BD 02, selective inhibitor of the first bromodomain of BRD4 (BRD4(1)) (IC50 = 382 nM). Exhibits 2-3-fold selectivity for BRD4(1) over the CBP bromodomain and has little affinity for a range of other bromodomains.
|
A16367 |
GW841819X |
BET 抑制剂 |
GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring 3.
|
A16368 |
BET-BAY 002 |
BET 抑制剂 |
BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.
|
A15876 |
PF-CBP1 |
CREBBP 抑制剂 |
PF-CBP1 is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.
|
A13451 |
PF-4 |
BRPF1 bromodomain 抑制剂 |
PFI-4 is a potent and selective and cell permeable BRPF1 bromodomain inhibitor (IC50 = 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4.
|
A12704 |
SF1126 |
Pan PI3K 抑制剂 |
SF1126 is a water soluble, small-molecule prodrug containing the pan-PI3K/mTOR inhibitor LY294002/SF1101 conjugated to the RGD-containing tetra-peptide SF1174 with potential antineoplastic and antiangiogenic activities.
|
A12815 |
C646 |
p300/CBP 抑制剂 |
C646 is a selective p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM).
|
A14015 SALE |
GSK2801 |
BAZ2A and BAZ2B 抑制剂 |
GSK2801 is a very potent inhibitor of the BAZ2 family of bromodomain containing proteins
|
A14160 SALE |
(-)-JQ1 |
BET bromodomain 抑制剂 |
The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes.
|
A14133 SALE |
GSK1324726A |
BET 抑制剂 |
GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM).
|
A14134 |
GSK 525768A |
- |
GSK 525768A is the enantiomer compound of GSK 525762A, which is a potent small molecule inhibitor that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4); GSK 525768A has NO activity towards BET.
|
A14226 |
Anacardic Acid |
KAT5 (Tip60), p300/PCAF 抑制剂 |
Anacardic Acid is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases.
|
A13957 |
PFI-3 |
SMARCA bromodomains probe |
PFI-3 is a selective chemical probe for SMARCA bromodomains.
|
A13956 SALE |
RVX-208 |
BET bromodomain 抑制剂 |
RVX-208 is a potent BET bromodomain inhibitor with IC50 of 0.510 uM for BD2, about 170-fold selectivity over BD1.
|
A15367 |
UNC 926 hydrochloride
|
MBT Domain (L3MBTL1) 抑制剂 |
UNC 926 is a methyl lysine reader domain inhibitor.
|
A16470 |
CPI-637 |
CBP/EP300 bromodomain 抑制剂 |
CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.
|